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Inhibition of P-Glycoprotein Mediated Efflux in Caco-2 Cells by Phytic Acid
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2018-01-16 00:00:00 , DOI: 10.1021/acs.jafc.7b04307 Lujia Li 1, 2 , Qingxue Fu 1, 3 , Mengxin Xia 1 , Lei Xin 1 , Hongyi Shen 1 , Guowen Li 2 , Guang Ji 4 , Qianchao Meng 5 , Yan Xie 1, 4
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2018-01-16 00:00:00 , DOI: 10.1021/acs.jafc.7b04307 Lujia Li 1, 2 , Qingxue Fu 1, 3 , Mengxin Xia 1 , Lei Xin 1 , Hongyi Shen 1 , Guowen Li 2 , Guang Ji 4 , Qianchao Meng 5 , Yan Xie 1, 4
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Phytic acid (IP6) is a natural phosphorylated inositol, which is abundantly present in most cereal grains and seeds. This study investigated the effects of IP6 regulation on P-glycoprotein (P-gp) and its potential mechanisms using in situ and in vitro models. The effective permeability of the typical P-gp substrate rhodamine 123 (R123) in colon was significantly increased from (1.69 ± 0.22) × 10–5 cm/s in the control group to (3.39 ± 0.417) × 10–5 cm/s (p < 0.01) in the 3.5 mM IP6 group. Additionally, IP6 can concentration-dependently decrease the R123 efflux ratio in both Caco-2 and MDCK II-MDR1 cell monolayers and increase intracellular R123 accumulation in Caco-2 cells. Furthermore, IP6 noncompetitively inhibited P-gp by impacting R123 efflux kinetics. The noncompetitive inhibition of P-gp by IP6 was likely due to decreases in P-gp ATPase activity and P-gp molecular conformational changes induced by IP6. In summary, IP6 is a promising P-gp inhibitor candidate.
中文翻译：
植酸抑制P-糖蛋白介导的Caco-2细胞外流
植酸（IP6）是一种天然的磷酸化肌醇，在大多数谷物和种子中都大量存在。这项研究使用原位和体外模型研究了IP6调节对P-糖蛋白（P-gp）的影响及其潜在机制。典型P-gp底物若丹明123（R123）在结肠中的有效渗透率从对照组的（1.69±0.22）×10 –5 cm / s显着增加到（3.39±0.417）×10 –5 cm / s （p<0.01）在3.5 mM IP6组中。此外，IP6可以浓度依赖性地降低Caco-2和MDCK II-MDR1细胞单层中的R123外流比率，并增加Caco-2细胞中的细胞内R123积累。此外，IP6通过影响R123外排动力学来非竞争性地抑制P-gp。IP6对P-gp的非竞争性抑制可能是由于IP6诱导的P-gp ATPase活性降低和P-gp分子构象变化。总之，IP6是有希望的P-gp抑制剂候选物。
更新日期：2018-01-16
中文翻译：
植酸抑制P-糖蛋白介导的Caco-2细胞外流
植酸（IP6）是一种天然的磷酸化肌醇，在大多数谷物和种子中都大量存在。这项研究使用原位和体外模型研究了IP6调节对P-糖蛋白（P-gp）的影响及其潜在机制。典型P-gp底物若丹明123（R123）在结肠中的有效渗透率从对照组的（1.69±0.22）×10 –5 cm / s显着增加到（3.39±0.417）×10 –5 cm / s （p<0.01）在3.5 mM IP6组中。此外，IP6可以浓度依赖性地降低Caco-2和MDCK II-MDR1细胞单层中的R123外流比率，并增加Caco-2细胞中的细胞内R123积累。此外，IP6通过影响R123外排动力学来非竞争性地抑制P-gp。IP6对P-gp的非竞争性抑制可能是由于IP6诱导的P-gp ATPase活性降低和P-gp分子构象变化。总之，IP6是有希望的P-gp抑制剂候选物。
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